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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

16.0K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

7.0K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
7.0K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

131.1K
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
131.1K
Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

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Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
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Protein Dynamics in Living Cells01:19

Protein Dynamics in Living Cells

2.5K
Different fluorescence-based techniques are used to study the protein dynamics in living cells. These techniques include FRAP, FRET, and PET.
Fluorescent recovery after photobleaching (FRAP) is a fluorescent-protein-based detection technique used to quantify protein movement rates within the cell. This method exposes a small portion of the cell to an intense laser beam. The laser beam causes permanent photobleaching of the fluorophore-tagged proteins in the exposed region. As the bleached...
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Related Experiment Video

Updated: Dec 23, 2025

Monitoring GPCR-&#946;-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
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Beyond structure: emerging approaches to study GPCR dynamics.

Anastasiia Gusach1, Ivan Maslov1, Aleksandra Luginina1

  • 1Research Center for Molecular Mechanisms of Aging and Age-Related Diseases, Moscow Institute of Physics and Technology, Dolgoprudny, 141700, Russia.

Current Opinion in Structural Biology
|April 20, 2020
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) are key membrane proteins in health and disease. Combining structural and dynamic studies is crucial for understanding complex GPCR signaling mechanisms and functions.

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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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Parallel Interrogation of &#946;-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) form the largest membrane protein superfamily.
  • GPCRs regulate critical physiological processes and are implicated in numerous diseases.
  • Recent advances have provided high-resolution structures of GPCRs with ligands and partners.

Purpose of the Study:

  • To review the integration of GPCR structure and dynamics studies.
  • To highlight how combined approaches advance understanding of GPCR signaling.
  • To explore key areas like biased agonism and allostery.

Main Methods:

  • Analysis of high-resolution structural data.
  • Integration of spectroscopic techniques for dynamics.
  • Review of current literature on GPCR structure-dynamics relationships.

Main Results:

  • Static structural snapshots alone are insufficient for full GPCR understanding.
  • GPCR dynamics provide essential insights into complex signaling.
  • Structure-dynamics interplay is key to understanding phenomena like biased agonism and allostery.

Conclusions:

  • Combining structural and dynamic studies is essential for a comprehensive understanding of GPCRs.
  • This integrated approach is critical for deciphering fundamental GPCR biology.
  • Future research should continue to leverage both structural and dynamic methodologies.